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0% within 24 h, and the metabolites were mainly excreted through the urine. In addition, the hypoglycemic activities of paeonol and its metabolites were investigated by a glucose uptake assay on TNF-α mediated insulin resistance in 3T3-L1 adipocytes. The results showed that paeonol and its major metabolites displayed hypoglycemic activities. This is the first comprehensive and systematic report on the pharmacokinetics of paeonol and its metabolites. This research provides an important basis for the clinical devel